反应详情

温度

0 °C

4-(7-Azaindol-5-yloxy)-6-methoxy-7-(3-piperazin-1-ylpropoxy)quinazoline (200 mg, 0.46 mmol) was dissolved in pyridine (5 ml) and cooled to 0° C. Trichloroacetyl isocyanate (55 μl, 0.46 mmol) was added and the mixture stirred at ambient temperature for 3 hours. The mixture was concentrated under reduced pressure and the residue dissolved in 7N ammonia in methanol and stirred at ambient temperature for 20 hours. The solvent was removed under reduced pressure and the residue was purified by column chromatography eluting with methylene chloride/methanol (90/10) to give 4-(7-azaindol-5-yloxy)-6-methoxy-7-[3-(4-carbamoylpiperazin-1-yl)propoxy]quinazoline (95 mg, 43%) as a white solid.

1. concentrationThe mixture was concentrated under reduced pressure
2. dissolutionthe residue dissolved in 7N ammonia in methanol
3. stirringstirred at ambient temperature for 20 hours
4. customThe solvent was removed under reduced pressure
5. customthe residue was purified by column chromatography
6. washeluting with methylene chloride/methanol (90/10)